26-09-2019 дата публикации
Номер: US20190292214A1
Embodiments of the invention are directed to new equatorially modified polymer linked multimers of guanosine-3′, 5′-cyclic monophosphate (cGMP) analogues that inhibit the cGMP-signaling system. The invention is also directed to related monomeric compounds, which may serve as monomeric precursors of the multimers, and/or also show itself inhibitory activity and/or impact the inhibitory activity of the related multimers. The invention further relates to the use of such compounds as reagents for signal transduction research and as modulators of cyclic nucleotide-regulated binding proteins and isoenzymes thereof, and as ligands for affinity chromatography, for antibody production or for diagnostic applications, e.g., on chip surfaces. 2. A compound according to claim 1 , wherein{'sup': 3', '4, 'in case of formula (I) Gand Gare absent'}or{'sup': 3', '4', '3', '4, 'in case of formula (II) G, G, LRand LRare absent.'}3. A compound according towherein{'sub': '8', 'all Rare SH.'}5. A compound according towherein{'sub': 1', '2', '2', '2, 'Rcan independently be H, halogen, azido, nitro, alkyl, acyl, aryl, OH, O-alkyl, O-aryl, SH, S-alkyl, S-aryl, S-aralkyl, S(O)-alkyl, S(O)-aryl, S(O)-aralkyl, S(O)-benzyl, S(O)-alkyl, S(O)-aryl, S(O)-aralkyl, amino, NH-alkyl, NH-aryl, NH-aralkyl, NR9R10, SiR13R14R15 wherein R9, R10, R13, R14, R15 are alkyl;'}and/or{'sub': 4', '5', '5', '5', '5, 'Rcan independently be absent, H, amino, alkyl, aralkyl, nitro, N-oxide or can form together with Y and Rand the carbon bridging Y and Ran imidazole ring which can be unsubstituted or substituted with alkyl, aryl or aralkyl, or can form together with Y and Rand the carbon bridging Y and Ran imidazolinone as depicted above (structure IV, V, n=1) or an homologous ring (n=2 to 8) which each can be unsubstituted or substituted (not depicted) with alkyl, aryl or aralkyl.'}and/or{'sub': 5', '4', '5', '4', '5, 'Rcan independently H, halogen, azido, acyl, aracyl, nitro, alkyl, aryl, aralkyl, amido-alkyl, amido- ...
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